title: Androgen receptor modulators: a marriage of chemistry and biology.
abstract: Androgenic steroids are important for male development in utero and secondary sexual characteristics at puberty. In addition, androgens play a role in non-reproductive tissues, such as bone and muscle in both sexes. The actions of the androgens testosterone and dihydrotestosterone are mediated by a single receptor protein, the androgen receptor. Over the last 60-70 years there has been considerable research interest in the development of inhibitors of androgen receptor for the management of diseases such as prostate cancer. However, more recently, there is also a growing appreciation of the need for selective androgen modulators that would demonstrate tissue-selective agonist or antagonist activity. The chemistry and biology of selective agonists, antagonists and selective androgen receptor modulators will be discussed in this review.
authors.affiliation: School of Medical Sciences, University of Aberdeen, Foresterhill, Aberdeen, AB25 2ZD, Scotland, UK. iain.mcewan@abdn.ac.uk
authors.forename: Iain J
authors.initials: IJ
authors.lastname: McEwan
mesh_terms: D000494:Allosteric Regulation; D045930:Anabolic Agents / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D059002:Androgen Receptor Antagonists / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D000728:Androgens / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D005260:Female; D006801:Humans; D008297:Male; D011085:Polycystic Ovary Syndrome / Q000188:drug therapy / Q000378:metabolism / Q000517:prevention & control; D011471:Prostatic Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000517:prevention & control; D011944:Receptors, Androgen / Q000737:chemistry / Q000378:metabolism*
chemical_list: D045930:Anabolic Agents; D059002:Androgen Receptor Antagonists; D000728:Androgens; D011944:Receptors, Androgen